Al 18F-PSMA-CM showed high PSMA specificity and accumulated in 22Rv1 tumors with increasing uptake in 4 h. Al 18F-PSMA-CM was accumulated in kidneys and 22Rv1 tumors, which were decreased by −80.0 and −84.3% when co-injected with ZJ-43. The Kd value of Al 18F-PSMA-CM to PSMA was 8.46 ± 0.24 nM. The uptake of Al 18F-PSMA-CM in PSMA(+) 22Rv1 cells was increased in 2 h, and the uptake was blocked by a PSMA inhibitor, ZJ-43. Al 18F-PSMA-CM was stable in vitro and in vivo and prolonged circulation in blood with a binding ratio of 47 ± 3.2% and Kd value of 3.08 ± 0.45 nM to HSA. Al 18F-PSMA-CM was prepared with a radiochemical purity of >99% and specific activity of 11.22–18.70 MBq/nmol.
Al 18F-PSMA-CM is evaluated in vitro and in vivo for stability, PSMA specificity, and biodistribution in 22Rv1 tumor-bearing mice. In this study, we introduced maleimidopropionic acid (MPA) to a PSMA-targeted tracer and developed Al 18F-PSMA-CM, which targets human serum albumin (HSA) binding and PSMA. Improving the circulation of radioligands in the blood is considered as an effective strategy that can improve tumor burden, which benefits detection of small lesions and improves the effect of PSMA radioligand therapy (PRLT). Prostate-specific membrane antigen (PSMA) is an attractive target for the diagnosis and therapy of prostate cancer as it is specifically overexpressed in prostate cancer cells.
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